N-Oxide heterocycles and imidazoles replacing ring D of calanolides against Mycobacterium tuberculosis  

作　　者：Zi-Jie Liu Xiao-Yong Guo Gang Liu 

机构地区：[1]Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College [2]Tsinghua-Peking Center for Life Sciences and Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University

出　　处：《Chinese Chemical Letters》2016年第1期51-54,共4页中国化学快报（英文版）

基　　金：supported by Bill and Melinda Gates Foundation Grant (No. OPP1024029);supported financially by the National Natural Science Foundation of China (No. 91213303)

摘　　要：We have explored the chemistry of N-oxide heterocycles and imidazoles replacing ring D of the natural product（＋）-calanolide A, and have synthesized 12 new analogues, two of which were active against both R Mtb and NR Mtb with MIC values of 12.5 mg/m L, which would lead to further optimization for more potent anti-TB candidates.We have explored the chemistry of N-oxide heterocycles and imidazoles replacing ring D of the natural product（＋）-calanolide A, and have synthesized 12 new analogues, two of which were active against both R Mtb and NR Mtb with MIC values of 12.5 mg/m L, which would lead to further optimization for more potent anti-TB candidates.

关 键 词：Mycobacterium tuberculosis （＋）-Calanolide A N-Oxide heterocycle Benzoimidazole Bioreductive drug 

分 类 号：O626[理学—有机化学] TQ460.1[理学—化学]